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Primary and metastatic tumors of the nervous system represent a diverse group of neoplasms, each characterized by distinct biological features, prognostic outcomes, and therapeutic approaches. Due to their molecular complexity and heterogeneity, nervous system cancers (NSCs) pose significant clinical challenges. For decades, plants and their natural products with established anticancer properties have played a pivotal role in the treatment of various medical conditions, including cancers. Anthraquinone derivatives, a class of tricyclic secondary metabolites, are found in several botanical families, such as Fabaceae, Polygonaceae, Rhamnaceae, and Rubiaceae. In a comprehensive review, recent advancements in the anticancer properties of 1,8-dihydroanthraquinone derivatives—such as emodin, aloe-emodin, hypericin, chrysophanol, rhein, and physcion—were analyzed. These compounds have been studied extensively, both used individually and in combination with other chemotherapeutic agents, using in vitro and in vivo models of nervous system tumors. It was demonstrated that 1,8-dihydroanthraquinone derivatives induce apoptosis and necrosis in cancerous cells, intercalate into DNA, disrupting transcription and replication in rapidly dividing cells, and alter ROS levels, leading to oxidative stress that damages tumor cells. Additionally, they can influence signaling pathways involved in oncogenesis, such as MAPK, PI3K/Akt, or others crucial for the survival and the proliferation of NSC cells. The exploration of 1,8-dihydroanthraquinone derivatives aims to develop novel therapies that could overcome resistance and improve cancer patients’ outcomes.

has a long history of medicinal use due to its diverse biological activities, including antioxidant, anti-inflammatory and antimicrobial. This study investigates the physicochemical and ADME (absorption, distribution, metabolism, excretion) properties of two primary anthraquinones from , aloin A and aloe-emodin. The focus of this research was to evaluate the lipophilicity, solubility, and pharmacokinetic profiles of aloin A and aloe-emodin through a combination of computational predictions, the shake-flask method, and chromatographic techniques. The optimised shake-flask method was successfully employed to determine the log values of phyto-chemicals. Aloin A was found to be more hydrophilic than aloe-emodin, likely due to the presence of an attached β-d-glucopyranosyl unit. All RP-TLC and RP-HPLC lipophilicity indices were higher for aloe-emodin compared to aloin A, aligning with their log values (obtained through and shake-flask methods). IAM (immobili sed artificial membrane)-HPLC results suggest that unlikely partitioning in the -octanol/water system or C18 chains, partition into phospholipids involves not only hydrophobic intermolecular recognition forces but also electrostatic interactions. The presence of a sugar moiety (β-d-glucopyranosyl unit) at the C-10 position of aloin A considerably enhanced its affinity to phospholipids compared to its affinity to alkyl chains. HSA (human serum albumin)-HPLC and AGP (α1-acid glycoprotein)-HPLC data confirmed aloe-emodin’s stronger affinity to plasma proteins. The integration of computational and experimental approaches provided a detailed understanding of aloin A and aloe-emodin physicochemical and ADME properties.

Neuropathic pain has been characterized as chronic pain resulting from pathological damage to the sensorimotor system. Because of its complex nature, it remains refractory to most of the therapeutic interventions, and surgical intervention and physiotherapy alongside steroidal treatments remain the only treatment protocols with limited success, hence solidifying the need to find efficacious therapeutic alternatives. Emodin was used as a post-treatment for its potential to be neuroprotective in the treatment of chronic constriction injury-induced NP. The first day following surgery, Emodin treatment began, and it lasted until the 21st day. On days 3, 7, 14 and 21, all behavioral investigations were conducted. The sciatic nerve and spinal cord were extracted for further molecular examination. Emodin elevated response latency, was able to delay the onset of mechanical hyperalgesia in rats on days 7, 14, and 21 and reduced the CCI-induced paw deformation. Emodin treatment significantly reduced lipid peroxidation and NO levels while restoring the GST, GSH and catalase. It significantly improved the disorientation of the sciatic nerve and spinal cord confirmed by H & E staining and reduced inflammatory markers as observed by the quantification of COX-2, TNF-α, p-NFκb and up-regulated PPAR-γ levels by ELISA and PCR. According to the findings, Emodin has antinociceptive and anti-hyperalgesic properties, which reduced pain perception and inflammation. We also suggested the involvement of PPAR-γ pathway in the therapeutic potential of emodin in chronic nerve injury.

Inflammatory diseases pose a major global health challenge, encompassing a wide range of chronic conditions driven by persistent inflammation. Emodin is a natural anthraquinone compound extracted from traditional Chinese medicinal herbs, exhibiting remarkable anti-inflammatory properties by regulating multiple inflammation-related signaling pathways. Despite its promising applications in the treatment of inflammatory diseases, issues such as poor water solubility, low bioavailability, rapid metabolism, and potential toxicity have limited its clinical translation. This review systematically reviews drug delivery systems (DDS) designed to overcome these limitations, with a focus on technological platforms including nanoparticles, liposomes, microspheres, nanocapsules, self-emulsifying systems, and microbubbles. Studies have shown that these platforms, through stimulus-responsive mechanisms and various targeting strategies, can significantly enhance emodin's solubility, stability, targeted delivery, and sustained-release effects, thereby improving bioavailability, reducing systemic toxicity, and strengthening anti-inflammatory efficacy. This review emphasizes the analysis of the design principles, mechanisms of action, and translational prospects of each system, while discussing challenges such as biocompatibility, stability, and scalable production, to fully exploit emodin's multi-target therapeutic potential and provide valuable references for researchers engaged in the development of anti-inflammatory DDS.

Cancers are generally recognized as the leading cause of death and a predominant barrier to prolonging life expectancy in both developed and developing countries. Emodin is a typical anthraquinone derivative from various plants that exhibits a wide spectrum of biological activities, such as anticancer, antibacterial, hepatoprotective and anti-inflammatory activities. Much previous preclinical evidence has demonstrated that emodin exhibits reliable effects on several cancer types, including lung cancer, liver cancer, colon cancer, breast cancer, pancreatic cancer, leukemia, cervical cancer, and ovarian cancer, . The related molecular mechanisms corresponding to the anticancer activities of emodin are involved in the induction of apoptosis, inhibition of cell proliferation, enhanced reactive oxygen species (ROS) accumulation, and induction of autophagy, . In the present review, we summarized the sources, anticancer properties and , molecular mechanisms, metabolic transformation and toxicities of emodin. In addition, we also discussed the limitations of the present investigations of emodin against cancers and gave some perspectives for them, which would be beneficial for the further exploration and development of this natural compound as a clinical cancer drug.

Methicillin-resistant Staphylococcus aureus (MRSA) is a serious and rapidly growing threat to human beings. Emodin has a potent activity against MRSA; however, its usage is limited due to high hydrophobicity and low oral bioavailability. Thus, the coaxial electrospinning nanofibers encapsulating emodin in the core of hydrophilic poly (vinylpyrrolidone), with a hygroscopic cellulose acetate sheath, have been fabricated to provide long-term effect against MRSA. Scanning electron microscopy and transmission electron microscopy confirmed the nanofibers had a linear morphology with nanometer in diameter, smooth surface, and core-shell structure. Attenuated total reflection-Fourier transform infrared spectra, X-ray diffraction patterns, and differential scanning calorimetric analyses verified emodin existed in amorphous form in the nanofibers. The nanofibers have 99.38 ± 1.00% entrapment efficiency of emodin and 167.8 ± 0.20% swelling ratio. Emodin released from nanofibers showed a biphasic drug release profile with an initial rapid release followed by a slower sustained release. CCK-8 assays confirmed the nontoxic nature of the emodin-loaded nanofibers to HaCaT cells. The anti-MRSA activity of the nanofibers can persist up to 9 days in AATCC147 and soft-agar overlay assays. These findings suggest that the emodin-loaded electrospun nanofibers with core-shell structure could be used as topical drug delivery system for wound infected by MRSA.

The most common host entry point of human adapted coronaviruses (CoV) including SARS-CoV-2 is through the initial colonization in the nostril and mouth region which is responsible for spread of the infection. Most recent studies suggest that the commercially available oral and nasal rinse products are effective in inhibiting the viral replication. However, the anti-viral mechanism of the active ingredients present in the oral rinses have not been studied. In the present study, we have assessed in vitro enzymatic inhibitory activity of active ingredients in the oral mouth rinse products: aloin A and B, chlorhexidine, eucalyptol, hexetidine, menthol, triclosan, methyl salicylate, sodium fluoride and povidone, against two important proteases of SARS-CoV-2 PLpro and 3CLpro. Our results indicate only aloin A and B effectively inhibited proteolytic activity of PLpro with an IC 50 of 13.16 and 16.08 μM. Interestingly, neither of the aloin isoforms inhibited 3CLpro enzymatic activity. Computational structural modelling of aloin A and B interaction with PLpro revealed that, both aloin isoforms form hydrogen bond with Tyr 268 of PLpro, which is critical for their proteolytic activity. Furthermore, 100 ns molecular dynamics (MD) simulation studies predicted that both aloin isoforms have strong interaction with Glu 167 , which is required for PLpro deubiquitination activity. Our results from the in vitro deubiquitinase inhibition assay show that aloin A and B isomers exhibit deubiquitination inhibitory activity with an IC 50 value of 15.68 and 17.51 µM, respectively. In conclusion, the isoforms of aloin inhibit both proteolytic and the deubiquitinating activity of SARS-CoV-2 PLpro, suggesting potential in inhibiting the replication of SARS-CoV-2 virus.

Docetaxel (DTX) resistance is the main cause of treatment failure in castration-resistant prostate cancer (CRPC). Pyrroline-5-carboxylic acid reductase 1 (PYCR1) is an enzyme involved in proline metabolism. It is highly expressed in various cancers and promotes malignant progression, yet its role in DTX resistance in prostate cancer remains unclear. In this study, bioinformatics analyses and / experiments demonstrated that interfering with PYCR1 expression modulates the sensitivity of prostate cancer cells to DTX. Subsequently, via structure-based virtual screening, molecular dynamics simulations, and cellular thermal shift assay (CETSA), emodin-an anthraquinone compound-was identified as a PYCR1-targeting agent. Collectively, these findings suggest that PYCR1 may serve as a key target mediating DTX resistance in prostate cancer, and the emodin-DTX combination provides a promising potential clinical strategy to overcome such resistance. Finally, its functions and safety were also verified through experiments.